Glucocorticoids - Adrenocortical Steroids Flashcards

15.10

1
Q

Class - Prednisone

A

Glucocorticoid; Immunosuppressive agent

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2
Q

MOA of Prednisone (3)

A

Prodrug that must be activated in the liver to prednisolone

4X stronger anti-inflammatory than cortisol and causes less Na+ retention in the kidneys

Intermediate duration of action

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3
Q

SE of Prednisone (4)

A

Glucose intolerance, immunosuppression, osteoporosis, psychosis

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4
Q

Class - Fludrocortisone

A

Glucocorticoid (used for mineralocorticoid purposes)

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5
Q

MOA of Fludrocortisone (2)

A

10X stronger anti-inflammatory than cortisol but causes 125X more Na+ retention in the kidneys

Short duration of action

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6
Q

When do you use Fludrocortisone?

A

Used in patients w/ hypoaldosteronism

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7
Q

SE of Fludrocortisone (9)

A

Adrenal suppression, fluid/electrolyte abnormalities, metabolic changes, edema, HTN, osteoporosis, growth suppression in children, cataracts, behavioral changes

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8
Q

Metabolic sides effects of Glucocorticoids (3)

A

Truncal obesity; muscle wasting (aka “Central sparing, peripheral wasting”); Cushing syndrome; osteoporosis

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9
Q

Anti-inflammatory/immunosuppressive effects of Glucocorticoids (4)

A
  1. Decreased arachidonic acid metabolism, both PGs and LTs (decreased COX-2 mRNA and protein, decreased PLA2 activity)
  2. Decreased cytokine expression
  3. Decreased cell-adhesion molecule expression
  4. Decreased fibroblast DNA synthesis/proliferation
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10
Q

Tissues that respond to glucocorticoids (7)

A
Adrenals 
Liver 
Kidney 
Brain/CNS 
Vasculature 
Muscle 
Adipose tissue
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11
Q

Tx of glucocorticoids (9)

A
Replacement therapy
Congenital adrenal hyperplasia (CAH)
Inflammatory states
Asthma
Immunosuppressive (transplant)
Skin diseases
Ulcerative colitis
Cancer chemotherapy
Thrombocytopenia
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12
Q

What drug is used to compare anti-inflammatory potency (GR) and Na+ retaining potency (MR)?

A

Cortisol; binds to MR and GR

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13
Q

What is the duration of action for cortisol?

A

short

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14
Q

Potency of Triamcinolone

A

5x Anti-inflammatory potency (GR)
0 Na+ retaining potency (MR)
Intermediate duration of action

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15
Q

Potency of Betamethasone

A

25x Anti-inflammatory potency (GR)
0 Na+ retaining potency (MR)
Long duration of action

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16
Q

Potency of Dexamethasone

A

25x Anti-inflammatory potency (GR)
0 Na+ retaining potency (MR)
Long duration of action

17
Q

What is the inactive conformation of cortisol?

A

Cortisone

18
Q

Can cortisone bind to MR and GR?

A

No, neither

19
Q

What converts cortisol to cortisone?

A

11 beta-HSD2

20
Q

What converts cortisone to cortisol?

A

11 beta-HSD1